Lanreotide is a marketed somatostatin analogue. It is a cyclic peptide with the amino acid sequence presented below:
wherein Nal is the abbreviation for naphthylalanine, and there is a disulfide bridge between the two cysteine residues.
Lanreotide is indicated in the treatment of acromegaly due to both pituitary and non-pituitary growth hormone-secreting tumors, the management of symptoms caused by neuroendocrine tumors (NET), particularly carcinoid tumors and VIPomas (VIP=Vasoactive Intestinal Peptide), and in the treatment of thyrotrophic adenoma.
The treatments require continuous or repeated administration to the patient over an extended period of time. As repeated injections cause both inconvenience and discomfort to the patient, sustained release preparations are desirable and have been the subject of development efforts. Thus lanreotide is available today in two formulations: a sustained release formulation which is injected intramuscularly every ten or fourteen days and an extended release formulation which is administered subcutaneously once a month or once every 2 months for certain acromegalic patients. However, even if this set of extended release formulations exists, a need remains to reduce both inconvenience and discomfort to the patient with extended release formulations covering more than 2 months or even 2 months for the patients not covered by the existing formulations.
To extend the duration of treatment for more than one month, in particular for at least two months, the amount of injected pharmaceutical active ingredient (injected dose) has to be increased. On the other hand, to avoid further discomfort for the patient, the injected volume must remain as low as possible and compatible with the parenteral administration route. Therefore, there is need for a new pharmaceutical composition of lanreotide capable of delivering a sustained release over at least two months, preferably with a high dose of lanreotide (e.g. 120, 240 or 360 mg) while keeping a convenient volume of injection (e.g. equal or less than 2 mL). The present invention provides such pharmaceutical compositions.